Insulin analogues with an acyl and aklylene glycol moiety

C - Chemistry – Metallurgy – 07 – K

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C07K 14/62 (2006.01) A61K 38/28 (2006.01)

Patent

CA 2695970

An acylated insulin analogue wherein the insulin analogue comprises a lysine residue connected C-terminally to the A21 amino acid residue or a peptide residue of up to 4 amino acid residues comprising a lysine residue which peptide residue is connected C-terminally to the A21 amino acid residue, characterized in that an acyl moiety comprising an alkylene glycol moiety is attached to the lysine residue in the A22 position or attached to a lysine residue present in the peptide residue that is attached to the C terminal end of the A21 amino acid residue and wherein there is only one lysine (K, Lys) in the insulin analogue, can conveniently be administered pulmonary.

L'invention porte sur un analogue de l'insuline acylé qui comprend un résidu lysine doté d'une liaison C-terminale à un résidu d'acide aminé A21, ou un résidu peptide comprenant jusqu'à 4 résidus acides aminés comprenant un résidu lysine, le résidu peptide étant doté d'une liaison C-terminale à un résidu acide aminé A21, caractérisé en ce qu'un fragment acyle comprenant un fragment alkylène glycol est attaché au résidu lysine en position A22 ou est attaché à un résidu lysine présent dans le résidu peptide qui est attaché à l'extrémité C-terminale du résidu acide aminé A21, et en ce que l'analogue de l'insuline ne comprend qu'une seule lysine (K, Lys), ledit analogue étant apte à être administré par voie pulmonaire.

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